摘要
目的合成抗抑郁药物阿戈美拉汀的两个杂质。方法以(7-甲氧基-1-萘基)乙腈为起始原料,经氢化、乙酰化、柱层析得阿戈美拉汀二聚乙酰胺(杂质A)。以2-(7-甲氧基-1-萘基)乙基胺为起始原料,制备阿戈美拉汀二聚尿素(杂质B)。结果两个目标化合物经1H NMR、13C NMR、MS确证其结构。结论合成的两个杂质可作为阿戈美拉汀质量控制对照品,本工艺操作可行,原料易得。
Objective To synthesize two impurities of antidepressant agomelatine. Methods Agomelatine dimer acetamide （impurity A） was synthesized via hydrogenation and acetylation, using （7-methoxy-l-naphthyl） acetonitrile as starting material, and the pure impurity was obtained by separation on columns. Agomelatine dimer urea （impurity B） was prepared via condensation, using 2-（7-methoxy-l-naphthyl） ethylamine as starting material. Results The structures of two impurities of agomelatine were verified by 1H NMR, 13C NMR and MS. Conclusion The two specified impurities can be used as reference substances of related substances in quality control of agomelatine. The reaction conditions are mild and the raw materials are cheap.
出处
《食品与药品》
CAS
2015年第6期400-403,共4页
Food and Drug
关键词
杂质
阿戈美拉汀
合成
impurity
agomelatine
synthesis
